Fluorine-containing optically active composition for anti-infection

A compound and anti-infection technology, applied in anti-infective drugs, organic active ingredients, organic chemistry, etc., can solve the problems of no clinical application significance, high toxicity, and large irritation of racemic ulifloxacin, and achieve no skin and muscle Stimulation, low side effects, strong biological activity
CN101550153AActive Publication Date: 2009-10-07GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTITUTE +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTITUTE
Publication Date
2009-10-07

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Abstract

The invention relates to a fluorine-containing optically active composition for anti-infection, in particular to a quinolones optically active fluorine-containing composition anti-infective drug, i.e. a quinolones optically active fluorine-containing composition 1 showed by a right formula, wherein HA in the right formula is organic acid or inorganic acid which can form a composition accepted by pharmacology with (S)-6-fluorine-1-methyl-4-oxo-7-(1-piperazinyl)-1H and 4H-(1, 3) sulfur azetidine combined with (3, 2-a) quinoline-3-carboxylic acid. The quinolones optically active fluorine-containing composition 1 has stable property; compared with ulifloxacin, the quinolones optically active fluorine-containing composition 1 improves the water solubility and lowers the pH value of a water solution, is easy to dissolve in water and has higher biological activity, little renal toxicity and no skin and muscle irritation; the drug level of unobserved untoward effect is 30 mg / kg and is enhanced by 10 times comparing with the ulifloxacin, thus the quinolones optically active fluorine-containing composition 1 has low side effect and wide antimicrobial spectrum, and the activity of the quinolones optically active fluorine-containing composition 1 is 1-3 times higher than that of the racemic ulifloxacin.
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Description

technical field

[0001] The invention relates to a quinolone optically active fluorine-containing compound anti-infective drug, in particular to (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H, 4H-[1,3]thiazetidino[3,2-a]quinoline-3-carboxylic acid forms pharmaceutically acceptable compounds with organic or inorganic acids. Background technique

[0002] Infectious disease is the most common clinical disease, involving almost all clinical specialties, and it is also one of the most common causes of patient death. According to the World Health Organization report in 2000, the number of deaths from infectious diseases was as high as 33.3% of the total number of deaths from various causes.

[0003] In the international market, quinolones account for about 18% of the market share of anti-infective drugs, with an average annual growth rate of 7%, and continue to grow at a high speed, ranking second only to β-lactam drugs in sales. Fluoroquinolones are also antibacterial drugs th...

Claims

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